1-乙酰基-4-溴-1H-吲唑合成路线 (共 12 条)
反应条件
1: hydrogenchloride; water / methanol / 7 h / 20 °C 2: potassium acetate; (1,1'-bis(diphenylphosphino)ferrocene)palladium(II) dichloride / dimethyl sulfoxide / 40 h / 80 °C / |Inert atmosphere View Scheme
参考文献
Genentech, Inc.; Heald, Robert Andrew; McLean, Neville James
Patent: US2014/65136 A1, 2014 ;
反应条件
1: hydrogenchloride / water; methanol / 7 h / 20 °C 2: potassium acetate / (1,1'-bis(diphenylphosphino)ferrocene)palladium(II) dichloride / dimethyl sulfoxide / 40 h / 80 °C / Inert atmosphere View Scheme
参考文献
Kim, Mi Kyoung; Shin, Heerim; Cho, Seo Young; Chong, Youhoon
Bioorganic and Medicinal Chemistry, 2014 , vol. 22, # 3 p. 1156 - 1162
反应条件
1: hydrogenchloride; water / methanol / 7 h / 20 °C 2: potassium acetate; (1,1'-bis(diphenylphosphino)ferrocene)palladium(II) dichloride / dimethyl sulfoxide / 40 h / 80 °C / |Inert atmosphere View Scheme
参考文献
Genentech, Inc.; Heald, Robert Andrew; McLean, Neville James
Patent: US2014/65136 A1, 2014 ;
反应条件
1: hydrogenchloride / water; methanol / 7 h / 20 °C 2: potassium acetate / (1,1'-bis(diphenylphosphino)ferrocene)palladium(II) dichloride / dimethyl sulfoxide / 40 h / 80 °C / Inert atmosphere 3: sodium hydrogencarbonate / bis-triphenylphosphine-palladium(II) chloride / toluene; ethanol; water / 1 h / 120 °C / Inert atmosphere; Microwave irradiation View Scheme
参考文献
WO2011/130628 A1, ;
WO 2011/130628 A1
反应条件
hydrogenchloride in methanol; water T=20°C; 7 h;
参考文献
WO2011/130628 A1, ;
Page/Page column 128 ;
WO 2011/130628 A1
反应条件
1: With potassium acetate in chloroform
T=0 - 20°C; 0.166667 h;
2: With 18-crown-6 ether; isopentyl nitrite
18 h;
参考文献
PIRAMED LIMITED
Patent: US2008/76768 A1, 2008 ;
Location in patent: Page/Page column 8 ;
反应条件
1: 3-bromo-2-methyl-phenylamine; acetic anhydride With potassium acetate in chloroform
T=0 - 20°C; 0.25 h;
2: isopentyl nitrite With 18-crown-6 ether in chloroform
T=65°C; 18 h;
参考文献
Kim, Mi Kyoung; Shin, Heerim; Cho, Seo Young; Chong, Youhoon
Bioorganic and Medicinal Chemistry, 2014 , vol. 22, # 3 p. 1156 - 1162
反应条件
1: With potassium acetate in toluene
T=60°C; 0.5 h;
2: With isopentyl nitrite in toluene
T=60°C; 18 h;
参考文献
Takeda Pharmaceutical Company Limited
Patent: EP2141150 A1, 2010 ;
Location in patent: Page/Page column 62-63 ;
反应条件
1: in chloroform
T=0 - 20°C; 0.166667 h;
2: With 18-crown-6 ether; isopentyl nitrite in chloroform
18 h; Heating / reflux; Product distribution / selectivity;
参考文献
GENENTECH, INC.; F. HOFFMANN-LA ROCHE AG
Patent: WO2009/146406 A1, 2009 ;
Location in patent: Page/Page column 63 ;
WO 2009/146406 A1
反应条件
1: With potassium acetate; acetic anhydride in chloroform
T=0 - 20°C; 0.166667 h;
2: With 18-crown-6 ether; isopentyl nitrite in chloroform
18 h; Heating / reflux; Product distribution / selectivity;
参考文献
Piramed Limited; Genentech, Inc.
Patent: US2008/76758 A1, 2008 ;
Location in patent: Page/Page column 74 ;
US 20080076758 A1